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Anti-microbial peptidomimetic compounds and methods to calculate anti-microbial activity

a technology of peptidomimetic compounds and anti-microbial activity, applied in the field of new molecules, can solve the problems of general no longer accepting that amps are uniform and indiscriminate, and achieve the effect of providing conformational flexibility for the backbon

Inactive Publication Date: 2012-05-29
USA AS REPRESENTED BY THE SEC OF THE ARMY ON BEHALF OF USAMRMC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

"The patent text describes a new approach to designing antimicrobial peptides (AMPs) that can target specific bacteria strains with increased potency and selectivity. The inventors have discovered that small changes in the structure and physicochemical properties of the constituent amino acids residues in the peptides can lead to major changes in their activity against different bacteria strains. By incorporating un-natural amino acids with specific physicochemical properties, the AMPs can exhibit increased resistance to proteolytic or enzymatic degradation and reduced hemolytic activity. The invention has also discovered that certain AMPs exhibit greater selectivity for certain bacteria strains. Overall, this approach provides a new way to develop effective drugs against drug-resistant bacteria."

Problems solved by technology

It is generally no longer accepted that AMPs are uniform and indiscriminant membrane detergents.

Method used

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  • Anti-microbial peptidomimetic compounds and methods to calculate anti-microbial activity
  • Anti-microbial peptidomimetic compounds and methods to calculate anti-microbial activity

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Embodiment Construction

Antimicrobial Peptides

[0271]To develop effective synthetic AMPs, the inventors selected analogs of the magainin family of host defense peptides because these peptides are active against Gram positive and negative bacteria, fungi and protozoa while exhibiting little mammalian cell toxicity.24 The interactions of the magainins25, 26 with membrane models have been extensively investigated resulting in the characterization of the magainins as well defined α-helical amphipathic cell-selective membrane-disruptors.16, 18, 19

[0272]The inventors previously reported two-dimensional NMR and molecular modeling.27 Investigations conducted in their laboratory indicated that (Ala 8,13,18)magainin-2-amide bound to dodecylphosphocholine (DPC) micelles adopts a α-helical structure involving residues 2 to 16 with the four C-terminal residues converging to a loose β-turn like structure. While (Ala8,13,18)magainin-2-amide bound to sodium dodecylsulfate (SDS) micelles adopts a α-helical structure involv...

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Abstract

This invention encompasses synthetic antimicrobial peptide analogs having certain un-natural amino acids, including the un-natural amino acids hydrophobic tetrahydroisoquinolinecarboxylic acid (Tic) and octahydroindolecarboxylic acid (Oic), incorporated into the polypeptide backbone. These antimicrobial peptides (AMPs) are useful to treat infection in humans and other mammals of such bacteria as Gram positive bacteria, Gram negative bacteria and Mycobacterium. Many of the AMPs also exhibit the property of reduced hemolytic activity. The invention also entails 3D-QSAR models and mathematical equations that calculate the biological activity of any peptide sequence against Staphylococcus aureus or Mycobacterium ranae.

Description

[0001]This application claims priority from U.S. provisional application 60 / 876,377, filed Dec. 21, 2006, the entire contents of which are incorporated herein by reference.FIELD OF THE INVENTION[0002]The focus of this application is novel membrane disruptive antimicrobial peptides (AMPs) with increased selectivity and potency against specific bacterial strains. As described below, this invention encompasses synthetic antimicrobial peptide analogs having certain formulas, including the un-natural hydrophobic amino acids tetrahydroisoquinolinecarboxylic acid (Tic) and octahydroindolecarboxylic acid (Oic). These antimicrobial peptides (AMPs) are useful to treat infection in humans and other mammals caused by such bacteria as Gram positive bacteria, Gram negative bacteria and Mycobacteria. Many of the AMPs also exhibit the property of reduced hemolytic activity.BACKGROUND OF THE INVENTION[0003]Antimicrobial peptides (AMP) have evolved in almost every class of living organism as a defens...

Claims

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Application Information

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Patent Type & Authority Patents(United States)
IPC IPC(8): A61K38/00C07K5/00C07K7/00C07K16/00C07K17/00G16B15/30
CPCC07K14/001C07K14/46G06F19/16A61K38/00G16B15/00A61P31/04G16B15/30
Inventor HICKS, RICKEY P.VENUGOPAL, DIVA KARAMENONBHONSLE, JAYENDRA
Owner USA AS REPRESENTED BY THE SEC OF THE ARMY ON BEHALF OF USAMRMC
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